CR20220241A - Inhibidores de ras - Google Patents

Inhibidores de ras

Info

Publication number
CR20220241A
CR20220241A CR20220241A CR20220241A CR20220241A CR 20220241 A CR20220241 A CR 20220241A CR 20220241 A CR20220241 A CR 20220241A CR 20220241 A CR20220241 A CR 20220241A CR 20220241 A CR20220241 A CR 20220241A
Authority
CR
Costa Rica
Prior art keywords
ras inhibitors
cancers
treatment
pharmaceutical compositions
protein complexes
Prior art date
Application number
CR20220241A
Other languages
English (en)
Inventor
G Leslie Burnett
Elena S Koltun
Adrian L Gill
James Aggen
Andreas Buckl
John E Knox
Yang Liu
Jennifer Pitzen
James Cregg
Original Assignee
Revolution Medicines Inc
Priority date (The priority date is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the date listed.)
Filing date
Publication date
Application filed by Revolution Medicines Inc filed Critical Revolution Medicines Inc
Publication of CR20220241A publication Critical patent/CR20220241A/es

Links

Classifications

    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D245/00—Heterocyclic compounds containing rings of more than seven members having two nitrogen atoms as the only ring hetero atoms
    • C07D245/04—Heterocyclic compounds containing rings of more than seven members having two nitrogen atoms as the only ring hetero atoms condensed with carbocyclic rings or ring systems
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D498/00—Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen and oxygen atoms as the only ring hetero atoms
    • C07D498/12—Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen and oxygen atoms as the only ring hetero atoms in which the condensed system contains three hetero rings
    • C07D498/18—Bridged systems
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00—Medicinal preparations containing organic active ingredients
    • A61K31/33—Heterocyclic compounds
    • A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/495—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with two or more nitrogen atoms as the only ring heteroatoms, e.g. piperazine or tetrazines
    • A61K31/50—Pyridazines; Hydrogenated pyridazines
    • A61K31/504—Pyridazines; Hydrogenated pyridazines forming part of bridged ring systems
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00—Medicinal preparations containing organic active ingredients
    • A61K31/33—Heterocyclic compounds
    • A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/535—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with at least one nitrogen and one oxygen as the ring hetero atoms, e.g. 1,2-oxazines
    • A61K31/5375—1,4-Oxazines, e.g. morpholine
    • A61K31/5377—1,4-Oxazines, e.g. morpholine not condensed and containing further heterocyclic rings, e.g. timolol
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00—Medicinal preparations containing organic active ingredients
    • A61K31/33—Heterocyclic compounds
    • A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/535—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with at least one nitrogen and one oxygen as the ring hetero atoms, e.g. 1,2-oxazines
    • A61K31/5375—1,4-Oxazines, e.g. morpholine
    • A61K31/5386—1,4-Oxazines, e.g. morpholine spiro-condensed or forming part of bridged ring systems
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00—Medicinal preparations containing organic active ingredients
    • A61K31/33—Heterocyclic compounds
    • A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/55—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having seven-membered rings, e.g. azelastine, pentylenetetrazole
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00—Antineoplastic agents
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D498/00—Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen and oxygen atoms as the only ring hetero atoms
    • C07D498/22—Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen and oxygen atoms as the only ring hetero atoms in which the condensed system contains four or more hetero rings
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D513/00—Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for in groups C07D463/00, C07D477/00 or C07D499/00 - C07D507/00
    • C07D513/22—Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for in groups C07D463/00, C07D477/00 or C07D499/00 - C07D507/00 in which the condensed system contains four or more hetero rings

Abstract

La descripción presenta compuestos macrocíclicos y composiciones farmacéuticas y complejos proteicos de los mismos, capaces de inhibir las proteínas Ras, y sus usos en el tratamiento de cánceres.
CR20220241A 2019-11-04 2020-11-04 Inhibidores de ras CR20220241A (es)

Applications Claiming Priority (6)

Application Number Priority Date Filing Date Title
US201962930355P 2019-11-04 2019-11-04
US201962951652P 2019-12-20 2019-12-20
US202063000357P 2020-03-26 2020-03-26
US202063011636P 2020-04-17 2020-04-17
US202063043588P 2020-06-24 2020-06-24
PCT/US2020/058841 WO2021091982A1 (en) 2019-11-04 2020-11-04 Ras inhibitors

Publications (1)

Publication Number Publication Date
CR20220241A true CR20220241A (es) 2022-08-03

Family

ID=73598995

Family Applications (1)

Application Number Title Priority Date Filing Date
CR20220241A CR20220241A (es) 2019-11-04 2020-11-04 Inhibidores de ras

Country Status (16)

Country Link
US (2) US11566007B2 (es)
EP (1) EP4054719A1 (es)
JP (1) JP2022553858A (es)
KR (1) KR20220109408A (es)
CN (2) CN115894606A (es)
AU (1) AU2020379734A1 (es)
BR (1) BR112022008565A2 (es)
CA (1) CA3159561A1 (es)
CL (1) CL2023000974A1 (es)
CO (1) CO2022006033A2 (es)
CR (1) CR20220241A (es)
IL (1) IL292644A (es)
MX (1) MX2022005359A (es)
PE (1) PE20221278A1 (es)
TW (1) TW202132316A (es)
WO (1) WO2021091982A1 (es)

Families Citing this family (33)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO2019217307A1 (en) 2018-05-07 2019-11-14 Mirati Therapeutics, Inc. Kras g12c inhibitors
EP3908283A4 (en) 2019-01-10 2022-10-12 Mirati Therapeutics, Inc. KRAS G12C INHIBITORS
US11453683B1 (en) 2019-08-29 2022-09-27 Mirati Therapeutics, Inc. KRas G12D inhibitors
JP2022548791A (ja) 2019-09-24 2022-11-21 ミラティ セラピューティクス， インコーポレイテッド 組み合わせ療法
JP2022553858A (ja) 2019-11-04 2022-12-26 レボリューション メディシンズ インコーポレイテッド Ｒａｓ阻害剤
CA3159559A1 (en) 2019-11-04 2021-05-14 Revolution Medicines, Inc. Ras inhibitors
US11608346B2 (en) 2019-11-04 2023-03-21 Revolution Medicines, Inc. Ras inhibitors
MX2022007515A (es) 2019-12-20 2022-09-19 Mirati Therapeutics Inc Inhibidores de sos1.
CR20230165A (es) 2020-09-15 2023-06-02 Revolution Medicines Inc Derivados indólicos como inhibidores de ras en el tratamiento del cáncer
WO2022133345A1 (en) 2020-12-18 2022-06-23 Erasca, Inc. Tricyclic pyridones and pyrimidones
WO2022235866A1 (en) 2021-05-05 2022-11-10 Revolution Medicines, Inc. Covalent ras inhibitors and uses thereof
CN117616031A (zh) 2021-05-05 2024-02-27 锐新医药公司 用于治疗癌症的ras抑制剂
BR112023022819A2 (pt) 2021-05-05 2024-01-16 Revolution Medicines Inc Compostos, composição farmacêutica, conjugados e métodos para tratar câncer em um sujeito, para tratar um distúrbio e para inibir uma proteína ras em uma célula
TW202313631A (zh) 2021-05-25 2023-04-01 美商銳新醫藥公司 抑制ｒａｓ之方法
WO2023015559A1 (en) * 2021-08-13 2023-02-16 Nutshell Biotech (Shanghai) Co., Ltd. Macrocycle compounds as inhibitors of ras
AR126854A1 (es) 2021-08-27 2023-11-22 Hoffmann La Roche Compuestos macrocíclicos para el tratamiento de cáncer
AR127308A1 (es) 2021-10-08 2024-01-10 Revolution Medicines Inc Inhibidores ras
WO2023086341A1 (en) 2021-11-09 2023-05-19 Biomea Fusion, Inc. Inhibitors of kras
WO2023103898A1 (zh) * 2021-12-07 2023-06-15 赛诺哈勃药业（成都）有限公司 具有clk和dyrk抑制活性的化合物、其制备方法及用途
WO2023114954A1 (en) 2021-12-17 2023-06-22 Genzyme Corporation Pyrazolopyrazine compounds as shp2 inhibitors
TW202330553A (zh) 2022-01-10 2023-08-01 美商銳新醫藥公司 Ｒａｓ抑制劑
EP4227307A1 (en) 2022-02-11 2023-08-16 Genzyme Corporation Pyrazolopyrazine compounds as shp2 inhibitors
WO2023172940A1 (en) 2022-03-08 2023-09-14 Revolution Medicines, Inc. Methods for treating immune refractory lung cancer
WO2023205701A1 (en) 2022-04-20 2023-10-26 Kumquat Biosciences Inc. Macrocyclic heterocycles and uses thereof
TW202400607A (zh) * 2022-04-25 2024-01-01 美商翰森生物有限責任公司 環狀化合物、製備方法及其醫藥用途
WO2023232776A1 (en) * 2022-06-01 2023-12-07 F. Hoffmann-La Roche Ag Haloindole macrocyclic compounds for the treatment of cancer
WO2023240263A1 (en) * 2022-06-10 2023-12-14 Revolution Medicines, Inc. Macrocyclic ras inhibitors
WO2024008610A1 (en) * 2022-07-04 2024-01-11 F. Hoffmann-La Roche Ag Macrocyclic inhibitors of kras for the treatment of cancer
WO2024008834A1 (en) * 2022-07-08 2024-01-11 F. Hoffmann-La Roche Ag Macrocycle compounds useful as kras inhibitors
WO2024040131A1 (en) 2022-08-17 2024-02-22 Treeline Biosciences, Inc. Pyridopyrimidine kras inhibitors
CN117903169A (zh) * 2022-09-19 2024-04-19 杭州阿诺生物医药科技有限公司 一种pan-KRAS抑制剂化合物
WO2024067857A1 (zh) * 2022-09-29 2024-04-04 南京明德新药研发有限公司 大环衍生物及其应用
WO2024081363A1 (en) 2022-10-12 2024-04-18 Revolution Medicines, Inc. Composition comprising a first ras inhibitor, second ras inhibitor and a shp2 inhibitor for use in the treatment of cancer

Family Cites Families (321)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
EP0290762B1 (en) 1984-10-04 1993-05-12 Sandoz Ag Cyclosporins
EP0194972B1 (en) 1985-03-11 1992-07-29 Sandoz Ag Novel cyclosporins
GB8827305D0 (en) 1988-11-23 1988-12-29 British Bio Technology Compounds
US6352694B1 (en) 1994-06-03 2002-03-05 Genetics Institute, Inc. Methods for inducing a population of T cells to proliferate using agents which recognize TCR/CD3 and ligands which stimulate an accessory molecule on the surface of the T cells
US5858358A (en) 1992-04-07 1999-01-12 The United States Of America As Represented By The Secretary Of The Navy Methods for selectively stimulating proliferation of T cells
US6534055B1 (en) 1988-11-23 2003-03-18 Genetics Institute, Inc. Methods for selectively stimulating proliferation of T cells
US6905680B2 (en) 1988-11-23 2005-06-14 Genetics Institute, Inc. Methods of treating HIV infected subjects
EP0393934B1 (en) 1989-04-15 1994-11-02 Nippon Chemiphar Co., Ltd. Novel peptides, and antidementia agents containing the same
PT98990A (pt) 1990-09-19 1992-08-31 American Home Prod Processo para a preparacao de esteres de acidos carboxilicos de rapamicina
US5120842A (en) 1991-04-01 1992-06-09 American Home Products Corporation Silyl ethers of rapamycin
US5100883A (en) 1991-04-08 1992-03-31 American Home Products Corporation Fluorinated esters of rapamycin
US5118678A (en) 1991-04-17 1992-06-02 American Home Products Corporation Carbamates of rapamycin
EP0584222B1 (en) 1991-05-10 1997-10-08 Rhone-Poulenc Rorer International (Holdings) Inc. Bis mono-and bicyclic aryl and heteroaryl compounds which inhibit egf and/or pdgf receptor tyrosine kinase
US5118677A (en) 1991-05-20 1992-06-02 American Home Products Corporation Amide esters of rapamycin
NZ243082A (en) 1991-06-28 1995-02-24 Ici Plc 4-anilino-quinazoline derivatives; pharmaceutical compositions, preparatory processes, and use thereof
US5151413A (en) 1991-11-06 1992-09-29 American Home Products Corporation Rapamycin acetals as immunosuppressant and antifungal agents
GB9125660D0 (en) 1991-12-03 1992-01-29 Smithkline Beecham Plc Novel compound
AU661533B2 (en) 1992-01-20 1995-07-27 Astrazeneca Ab Quinazoline derivatives
ES2089723T3 (es) 1992-03-27 1996-10-01 American Home Prod 29-demetoxirapamicina para inducir la inmunodepresion.
US5521184A (en) 1992-04-03 1996-05-28 Ciba-Geigy Corporation Pyrimidine derivatives and processes for the preparation thereof
ZA935112B (en) 1992-07-17 1994-02-08 Smithkline Beecham Corp Rapamycin derivatives
ZA935111B (en) 1992-07-17 1994-02-04 Smithkline Beecham Corp Rapamycin derivatives
US5256790A (en) 1992-08-13 1993-10-26 American Home Products Corporation 27-hydroxyrapamycin and derivatives thereof
GB9221220D0 (en) 1992-10-09 1992-11-25 Sandoz Ag Organic componds
US5258389A (en) 1992-11-09 1993-11-02 Merck & Co., Inc. O-aryl, O-alkyl, O-alkenyl and O-alkynylrapamycin derivatives
JP3560609B2 (ja) 1992-11-13 2004-09-02 イミュネックス・コーポレーション Ｅｌｋリガンドと呼ばれる新規なサイトカイン
US5455258A (en) 1993-01-06 1995-10-03 Ciba-Geigy Corporation Arylsulfonamido-substituted hydroxamic acids
GB9303681D0 (en) 1993-02-24 1993-04-14 Pitman Moore Inc Vaccines
US5516658A (en) 1993-08-20 1996-05-14 Immunex Corporation DNA encoding cytokines that bind the cell surface receptor hek
WO1995008548A1 (en) 1993-09-20 1995-03-30 The Leland Stanford Junior University Recombinant production of novel polyketides
US5612340A (en) 1993-10-01 1997-03-18 Ciba-Geigy Corporation Pyrimidineamine derivatives and processes for the preparation thereof
US5656643A (en) 1993-11-08 1997-08-12 Rhone-Poulenc Rorer Pharmaceuticals Inc. Bis mono-and bicyclic aryl and heteroaryl compounds which inhibit EGF and/or PDGF receptor tyrosine kinase
EP0729471A1 (en) 1993-11-19 1996-09-04 Abbott Laboratories Semisynthetic analogs of rapamycin (macrolides) being immunomodulators
DE69423781T2 (de) 1993-12-17 2000-08-10 Novartis Ag Rapamycin-derivate als immunosuppressoren
US5700823A (en) 1994-01-07 1997-12-23 Sugen, Inc. Treatment of platelet derived growth factor related disorders such as cancers
IL112248A0 (en) 1994-01-25 1995-03-30 Warner Lambert Co Tricyclic heteroaromatic compounds and pharmaceutical compositions containing them
IL112249A (en) 1994-01-25 2001-11-25 Warner Lambert Co Pharmaceutical compositions containing di and tricyclic pyrimidine derivatives for inhibiting tyrosine kinases of the epidermal growth factor receptor family and some new such compounds
AU2096895A (en) 1994-03-07 1995-09-25 Sugen, Incorporated Receptor tyrosine kinase inhibitors for inhibiting cell proliferative disorders and compositions thereof
IL112873A (en) 1994-03-08 2005-03-20 Wyeth Corp Rapamycin-fkbp12 binding proteins, their isolation and their use
EP1464706A3 (en) 1994-04-15 2004-11-03 Amgen Inc., HEK5, HEK7, HEK8, HEK11, EPH-like receptor protein tyrosine kinases
DK0682027T3 (da) 1994-05-03 1998-05-04 Ciba Geigy Ag Pyrrolopyrimidinderivater med antiproliferativ virkning
GB9410142D0 (en) 1994-05-20 1994-07-06 Univ Warwick Carbapenems
US7175843B2 (en) 1994-06-03 2007-02-13 Genetics Institute, Llc Methods for selectively stimulating proliferation of T cells
US6303769B1 (en) 1994-07-08 2001-10-16 Immunex Corporation Lerk-5 dna
US5919905A (en) 1994-10-05 1999-07-06 Immunex Corporation Cytokine designated LERK-6
GB9524630D0 (en) 1994-12-24 1996-01-31 Zeneca Ltd Chemical compounds
US6057124A (en) 1995-01-27 2000-05-02 Amgen Inc. Nucleic acids encoding ligands for HEK4 receptors
US5863949A (en) 1995-03-08 1999-01-26 Pfizer Inc Arylsulfonylamino hydroxamic acid derivatives
WO1996030347A1 (en) 1995-03-30 1996-10-03 Pfizer Inc. Quinazoline derivatives
DK0819129T3 (da) 1995-04-03 2000-10-23 Novartis Ag Pyrazolderivater og fremgangsmåde til deres fremstilling
CA2218503C (en) 1995-04-20 2001-07-24 Pfizer Inc. Arylsulfonyl hydroxamic acid derivatives
GB9508538D0 (en) 1995-04-27 1995-06-14 Zeneca Ltd Quinazoline derivatives
US6692964B1 (en) 1995-05-04 2004-02-17 The United States Of America As Represented By The Secretary Of The Navy Methods for transfecting T cells
US7067318B2 (en) 1995-06-07 2006-06-27 The Regents Of The University Of Michigan Methods for transfecting T cells
US5747498A (en) 1996-05-28 1998-05-05 Pfizer Inc. Alkynyl and azido-substituted 4-anilinoquinazolines
US5650415A (en) 1995-06-07 1997-07-22 Sugen, Inc. Quinoline compounds
DE69624921T2 (de) 1995-06-09 2003-09-11 Novartis Ag Rapamycinderivate
US5624677A (en) 1995-06-13 1997-04-29 Pentech Pharmaceuticals, Inc. Controlled release of drugs delivered by sublingual or buccal administration
US6124453A (en) 1995-07-04 2000-09-26 Novartis Ag Macrolides
CZ1598A3 (cs) 1995-07-06 1998-04-15 Novartis Ag Pyrrolopyrimidiny a způsoby jejich přípravy
AR004010A1 (es) 1995-10-11 1998-09-30 Glaxo Group Ltd Compuestos heterociclicos
GB9523675D0 (en) 1995-11-20 1996-01-24 Celltech Therapeutics Ltd Chemical compounds
ATE225343T1 (de) 1995-12-20 2002-10-15 Hoffmann La Roche Matrix-metalloprotease inhibitoren
EP0888349B1 (en) 1996-01-23 2002-05-22 Novartis AG Pyrrolopyrimidines and processes for their preparation
JP3406763B2 (ja) 1996-01-30 2003-05-12 東レ・ダウコーニング・シリコーン株式会社 シリコーンゴム組成物
GB9603097D0 (en) 1996-02-14 1996-04-10 Zeneca Ltd Quinazoline compounds
GB9603095D0 (en) 1996-02-14 1996-04-10 Zeneca Ltd Quinazoline derivatives
DE19629652A1 (de) 1996-03-06 1998-01-29 Thomae Gmbh Dr K 4-Amino-pyrimidin-Derivate, diese Verbindungen enthaltende Arzneimittel, deren Verwendung und Verfahren zu ihrer Herstellung
DE19608588A1 (de) 1996-03-06 1997-09-11 Thomae Gmbh Dr K Pyrimido [5,4-d]pyrimidine, diese Verbindungen enthaltende Arzneimittel, deren Verwendung und Verfahren zu ihrer Herstellung
BR9709443B1 (pt) 1996-03-15 2009-05-05 n-7-heterociclil-pirrol[2,3-d]pirimidinas, bem como composições farmacêuticas compreendendo as mesmas.
CN100503580C (zh) 1996-04-12 2009-06-24 沃尼尔·朗伯公司 酪氨酸激酶的不可逆抑制剂
GB9607729D0 (en) 1996-04-13 1996-06-19 Zeneca Ltd Quinazoline derivatives
BR9709959A (pt) 1996-06-24 2000-05-09 Pfizer Derivados tricìclicos de fenilamino substituìdo para o tratamento de doenças hiperproliferativas
PL331285A1 (en) 1996-07-05 1999-07-05 Biotica Tech Ltd Erythromycins and method of preparing them
EP0818442A3 (en) 1996-07-12 1998-12-30 Pfizer Inc. Cyclic sulphone derivatives as inhibitors of metalloproteinases and of the production of tumour necrosis factor
EP0937082A2 (en) 1996-07-12 1999-08-25 Ariad Pharmaceuticals, Inc. Materials and method for treating or preventing pathogenic fungal infection
HRP970371A2 (en) 1996-07-13 1998-08-31 Kathryn Jane Smith Heterocyclic compounds
BR9710362A (pt) 1996-07-13 1999-08-17 Glaxo Group Ltd Composto formula-ao farmaceutica utiliza-ao de um composto processos de tratamento de um ser humano ou animal sofrendo de uma mediada por atividade anormal de cinase de proteina tirosina e para a prepara-ao de um composto
DE69716916T2 (de) 1996-07-13 2003-07-03 Glaxo Group Ltd Kondensierte heterozyklische verbindungen als protein kinase inhibitoren
DE69712496T2 (de) 1996-07-18 2002-08-29 Pfizer Matrix metalloprotease-inhibitoren auf basis von phosphinsäuren
US6111090A (en) 1996-08-16 2000-08-29 Schering Corporation Mammalian cell surface antigens; related reagents
EP1947183B1 (en) 1996-08-16 2013-07-17 Merck Sharp & Dohme Corp. Mammalian cell surface antigens; related reagents
DK0938486T3 (da) 1996-08-23 2008-07-07 Novartis Ag Substituerede pyrrolopyrimidiner og fremgangsmåder til deres fremstilling
KR20000068248A (ko) 1996-08-23 2000-11-25 디. 제이. 우드, 스피겔 알렌 제이 아릴설포닐아미노 하이드록삼산 유도체
SE9603465D0 (sv) 1996-09-23 1996-09-23 Astra Ab New compounds
WO1998014450A1 (en) 1996-10-02 1998-04-09 Novartis Ag Pyrimidine derivatives and processes for the preparation thereof
AU4779897A (en) 1996-10-02 1998-04-24 Novartis Ag Fused pyrazole derivatives and processes for their preparation
ID18494A (id) 1996-10-02 1998-04-16 Novartis Ag Turunan pirazola leburan dan proses pembuatannya
EP0837063A1 (en) 1996-10-17 1998-04-22 Pfizer Inc. 4-Aminoquinazoline derivatives
GB9621757D0 (en) 1996-10-18 1996-12-11 Ciba Geigy Ag Phenyl-substituted bicyclic heterocyclyl derivatives and their use
PT950059E (pt) 1997-01-06 2004-10-29 Pfizer Derivados de sulfona ciclicos
US6303636B1 (en) 1997-02-03 2001-10-16 Pfizer Inc Arylsulfonylamino hydroxamic acid derivatives
WO1998033798A2 (en) 1997-02-05 1998-08-06 Warner Lambert Company Pyrido[2,3-d]pyrimidines and 4-amino-pyrimidines as inhibitors of cell proliferation
AU5493598A (en) 1997-02-07 1998-08-26 Pfizer Inc. N-hydroxy-beta-sulfonyl-propionamide derivatives and their use as inhibitors of matrix metalloproteinases
BR9807678A (pt) 1997-02-11 2000-02-15 Pfizer Derivados de ácidos arilsulfonil-hidroxâmicos
CO4950519A1 (es) 1997-02-13 2000-09-01 Novartis Ag Ftalazinas, preparaciones farmaceuticas que las comprenden y proceso para su preparacion
US6902913B2 (en) 1997-04-30 2005-06-07 Kosan Biosciences, Inc. Recombinant narbonolide polyketide synthase
US6150395A (en) 1997-05-30 2000-11-21 The Regents Of The University Of California Indole-3-carbinol (I3C) derivatives and methods
US6329375B1 (en) 1997-08-05 2001-12-11 Sugen, Inc. Tricyclic quinoxaline derivatives as protein tyrosine kinase inhibitors
CA2299355C (en) 1997-08-08 2005-09-27 Pfizer Products Inc. Aryloxyarylsulfonylamino hydroxamic acid derivatives
US6509173B1 (en) 1997-10-21 2003-01-21 Human Genome Sciences, Inc. Human tumor necrosis factor receptor-like proteins TR11, TR11SV1, and TR11SV2
GB9725782D0 (en) 1997-12-05 1998-02-04 Pfizer Ltd Therapeutic agents
US6153383A (en) 1997-12-09 2000-11-28 Verdine; Gregory L. Synthetic transcriptional modulators and uses thereof
GB9800569D0 (en) 1998-01-12 1998-03-11 Glaxo Group Ltd Heterocyclic compounds
GB9800575D0 (en) 1998-01-12 1998-03-11 Glaxo Group Ltd Heterocyclic compounds
JP2002502607A (ja) 1998-02-09 2002-01-29 ジェネンテク・インコーポレイテッド 新規な腫瘍壊死因子レセプター相同体及びそれをコードする核酸
WO1999045009A1 (en) 1998-03-04 1999-09-10 Bristol-Myers Squibb Company Heterocyclo-substituted imidazopyrazine protein tyrosine kinase inhibitors
PA8469401A1 (es) 1998-04-10 2000-05-24 Pfizer Prod Inc Derivados biciclicos del acido hidroxamico
PA8469501A1 (es) 1998-04-10 2000-09-29 Pfizer Prod Inc Hidroxamidas del acido (4-arilsulfonilamino)-tetrahidropiran-4-carboxilico
US6372712B1 (en) 1998-05-22 2002-04-16 The Board Of Trustees Of The Leland Stanford Jr. University Synthetic bifunctional molecules containing a drug moiety and presenter protein ligand
WO1999061422A1 (en) 1998-05-29 1999-12-02 Sugen, Inc. Pyrrole substituted 2-indolinone protein kinase inhibitors
UA60365C2 (uk) 1998-06-04 2003-10-15 Пфайзер Продактс Інк. Похідні ізотіазолу, спосіб їх одержання, фармацевтична композиція та спосіб лікування гіперпроліферативного захворювання у ссавця
EP1097147A4 (en) 1998-07-10 2001-11-21 Merck & Co Inc NEW ANGIOGENESIS INHIBITORS
CA2341409A1 (en) 1998-08-31 2000-03-09 Merck And Co., Inc. Novel angiogenesis inhibitors
WO2000020601A2 (en) 1998-10-02 2000-04-13 Kosan Biosciences, Inc. Polyketide synthase enzymes and recombinant dna constructs therefor
US6686454B1 (en) 1998-10-09 2004-02-03 Isotechnika, Inc. Antibodies to specific regions of cyclosporine related compounds
EP1004578B1 (en) 1998-11-05 2004-02-25 Pfizer Products Inc. 5-oxo-pyrrolidine-2-carboxylic acid hydroxamide derivatives
US6753173B1 (en) 1999-02-09 2004-06-22 Board Of Trustees Of The Leland Stanford Junior University Methods to mediate polyketide synthase module effectiveness
CA2366857C (en) 1999-03-30 2010-12-14 Novartis Ag Phthalazine derivatives for treating inflammatory diseases
GB9912961D0 (en) 1999-06-03 1999-08-04 Pfizer Ltd Metalloprotease inhibitors
NZ516258A (en) 1999-06-07 2004-02-27 Immunex Corp Tek antagonists
US6521424B2 (en) 1999-06-07 2003-02-18 Immunex Corporation Recombinant expression of Tek antagonists
DE60036945T2 (de) 1999-07-12 2008-08-21 Genentech, Inc., South San Francisco Stimulierung oder hemmung von angiogenese und herzvaskularisierung mit tumor nekrose faktor ligand/rezeptor homologen
CN1293081C (zh) 1999-08-24 2007-01-03 阿里亚德基因治疗公司 28－表雷帕霉素类似物,其制备方法，药物组合物和用途
DK1676845T3 (da) 1999-11-05 2008-09-15 Astrazeneca Ab Nye quinazolinderivater
GB9927191D0 (en) 1999-11-17 2000-01-12 Angeletti P Ist Richerche Bio Methods and means for regulation of gene expression
US7220552B1 (en) 1999-11-19 2007-05-22 The Board Of Trustees Of The Leland Stanford Junior University Bifunctional molecules and their use in the disruption of protein-protein interactions
EP1230353A4 (en) 1999-11-19 2002-11-06 Univ Leland Stanford Junior BIFUNCTIONAL MOLECULES AND THEIR USE FOR INHIBITING PROTEIN-PROTEIN INTERACTIONS
DK1233943T3 (da) 1999-11-24 2011-08-15 Sugen Inc Ioniserbare indolinon derivater og anvendelse deraf som PTK ligander
US6515004B1 (en) 1999-12-15 2003-02-04 Bristol-Myers Squibb Company N-[5-[[[5-alkyl-2-oxazolyl]methyl]thio]-2-thiazolyl]-carboxamide inhibitors of cyclin dependent kinases
US6727225B2 (en) 1999-12-20 2004-04-27 Immunex Corporation TWEAK receptor
JP4902925B2 (ja) 2000-02-08 2012-03-21 シンヴェント エイエス ナイスタチンポリケチドシンターゼをコードする新規の遺伝子、およびそれらの取扱ならびに用途
US6797514B2 (en) 2000-02-24 2004-09-28 Xcyte Therapies, Inc. Simultaneous stimulation and concentration of cells
US6867041B2 (en) 2000-02-24 2005-03-15 Xcyte Therapies, Inc. Simultaneous stimulation and concentration of cells
MXPA02008265A (es) 2000-02-24 2004-09-10 Xcyte Therapies Inc Concentracion y estimulacion simultanea de calulas.
US7572631B2 (en) 2000-02-24 2009-08-11 Invitrogen Corporation Activation and expansion of T cells
AU2001247219B2 (en) 2000-02-25 2007-01-04 Immunex Corporation Integrin antagonists
EP1283827A2 (en) 2000-05-23 2003-02-19 Vertex Pharmaceuticals Incorporated Caspase inhibitors and uses thereof
US7176037B2 (en) 2000-07-13 2007-02-13 The Scripps Research Institute Labeled peptides, proteins and antibodies and processes and intermediates useful for their preparation
US6630500B2 (en) 2000-08-25 2003-10-07 Cephalon, Inc. Selected fused pyrrolocarbazoles
CZ304059B6 (cs) 2000-12-21 2013-09-11 Glaxo Group Limited Deriváty pyrimidinu a farmaceutický prostredek
US6995162B2 (en) 2001-01-12 2006-02-07 Amgen Inc. Substituted alkylamine derivatives and methods of use
US6878714B2 (en) 2001-01-12 2005-04-12 Amgen Inc. Substituted alkylamine derivatives and methods of use
US7102009B2 (en) 2001-01-12 2006-09-05 Amgen Inc. Substituted amine derivatives and methods of use
US20020147198A1 (en) 2001-01-12 2002-10-10 Guoqing Chen Substituted arylamine derivatives and methods of use
US7105682B2 (en) 2001-01-12 2006-09-12 Amgen Inc. Substituted amine derivatives and methods of use
WO2003014311A2 (en) 2001-08-06 2003-02-20 Kosan Biosciences, Inc. Methods for altering polyketide synthase genes
US6809077B2 (en) 2001-10-12 2004-10-26 Enanta Pharmaceuticals, Inc. Cyclosporin analogs for the treatment of autoimmune diseases
US6987090B2 (en) 2002-05-09 2006-01-17 Lg Household & Health Care Ltd. Use of 3-position cyclosporin derivatives for hair growth
US7307088B2 (en) 2002-07-09 2007-12-11 Amgen Inc. Substituted anthranilic amide derivatives and methods of use
TWI329112B (en) 2002-07-19 2010-08-21 Bristol Myers Squibb Co Novel inhibitors of kinases
US7012065B2 (en) 2003-02-07 2006-03-14 Enanta Pharmaceuticals, Inc. Cyclosporins for the treatment of immune disorders
EP1477563A3 (en) 2003-05-16 2004-11-24 Wyeth Cloning genes from streptomyces cyaneogriseus subsp.noncyanogenus for biosynthesis of antibiotics and methods of use
KR20060052681A (ko) 2003-05-23 2006-05-19 와이어쓰 Ｇｉｔｒ 리간드, ｇｉｔｒ 리간드-연관 분자, 항체 및그의 용도
ES2316995T3 (es) 2003-07-08 2009-04-16 Novartis Ag Uso de rapamicina y derivados de rapamicida para el tratamiento de la perdida osea.
WO2005007190A1 (en) 2003-07-11 2005-01-27 Schering Corporation Agonists or antagonists of the clucocorticoid-induced tumour necrosis factor receptor (gitr) or its ligand for the treatment of immune disorders, infections and cancer
WO2005016252A2 (en) 2003-07-11 2005-02-24 Ariad Gene Therapeutics, Inc. Phosphorus-containing macrocycles
TW200523262A (en) 2003-07-29 2005-07-16 Smithkline Beecham Corp Inhibitors of AKT activity
SG145749A1 (en) 2003-08-15 2008-09-29 Novartis Ag 2, 4-pyrimidinediamines useful in the treatment of neoplastic diseases, inflammatory and immune system disorders
JP2007518399A (ja) 2003-12-02 2007-07-12 ジェンザイム コーポレイション 肺癌を診断および治療する組成物並びに方法
WO2005094314A2 (en) 2004-03-26 2005-10-13 The Burnham Institute Modulators of shp2 tyrosine phosphatase and their use in the treatment of body weight disorders
GB0409799D0 (en) 2004-04-30 2004-06-09 Isis Innovation Method of generating improved immune response
US20060002932A1 (en) 2004-06-04 2006-01-05 Duke University Methods and compositions for enhancement of immunity by in vivo depletion of immunosuppressive cell activity
CN101023064B (zh) 2004-08-26 2011-02-16 辉瑞大药厂 作为蛋白激酶抑制剂的对映异构体纯的氨基杂芳基化合物
GT200500287A (es) 2004-10-13 2006-04-17 Analogos de 17-hidroxiwortmanina como inhibidores de pi3k
DK1866339T3 (da) 2005-03-25 2013-09-02 Gitr Inc GTR-bindende molekyler og anvendelser heraf
DK2161336T4 (en) 2005-05-09 2017-04-24 Ono Pharmaceutical Co Human monoclonal antibodies for programmed death 1 (PD-1) and methods for treating cancer using anti-PD-1 antibodies alone or in combination with other immunotherapies
GB0510390D0 (en) 2005-05-20 2005-06-29 Novartis Ag Organic compounds
WO2007034327A1 (en) 2005-09-20 2007-03-29 Pfizer Products Inc. Dosage forms and methods of treatment using a tyrosine kinase inhibitor
EP1981969A4 (en) 2006-01-19 2009-06-03 Genzyme Corp ANTI-GITRANT ANTIBODIES FOR THE TREATMENT OF CANCER
BRPI0708299A2 (pt) 2006-02-27 2011-05-24 Univ Leland Stanford Junior composições e métodos para o transporte de moléculas com propriedades melhoradas de liberação através de barreiras biológicas
US20070203168A1 (en) 2006-02-28 2007-08-30 Zhao Jonathon Z Isomers of rapamycin and 42-Epi-rapamycin, methods of making and using the same
WO2007117699A2 (en) 2006-04-07 2007-10-18 University Of South Florida Inhibition of shp2/ptpn11 protein tyrosine phosphatase by nsc-87877, nsc-117199 and their analogs
US7601852B2 (en) 2006-05-11 2009-10-13 Kosan Biosciences Incorporated Macrocyclic kinase inhibitors
TWI499420B (zh) 2006-12-07 2015-09-11 Hoffmann La Roche 肌醇磷脂３-激酶抑制劑化合物及使用方法
WO2008124815A1 (en) 2007-04-10 2008-10-16 University Of South Florida Method of activating nk cells
US8591886B2 (en) 2007-07-12 2013-11-26 Gitr, Inc. Combination therapies employing GITR binding molecules
RU2523890C2 (ru) 2007-09-12 2014-07-27 Дженентек, Инк. Комбинации ингибиторов фосфоинозитид 3-киназы и химиотерапевтических агентов и способы применения
WO2009049098A2 (en) 2007-10-09 2009-04-16 Indiana University Research & Technology Corporation Materials and methods for regulating the activity of phosphatases
KR100945483B1 (ko) 2007-10-25 2010-03-05 이화여자대학교 산학협력단 ｐｉｋＤ 조절유전자의 발현벡터를 이용한 스트렙토미세스베네주엘라에（Ｓｔｒｅｐｔｏｍｙｃｅｓｖｅｎｅｚｕｅｌａｅ）에서폴리케타이드（ｐｏｌｙｋｅｔｉｄｅ）의 생산성 증가방법
JP5348725B2 (ja) 2007-10-25 2013-11-20 ジェネンテック， インコーポレイテッド チエノピリミジン化合物の製造方法
GB0805363D0 (en) 2008-03-20 2008-04-30 Sinvent As Novel NRPS-PKS gene cluster and its manipulation and utility
WO2009135000A2 (en) 2008-04-30 2009-11-05 H. Lee Moffitt Cancer Center And Research Institute, Inc. Inhibition of shp2/ptpn11 protein tyrosine phosphatase by nsc-117199 and analogs
WO2010003118A1 (en) 2008-07-02 2010-01-07 Trubion Pharmaceuticals, Inc. Tgf-b antagonist multi-target binding proteins
WO2010011666A2 (en) 2008-07-21 2010-01-28 University Of South Florida Indoline scaffold shp-2 inhibitors and cancer treatment method
WO2010030002A1 (ja) 2008-09-12 2010-03-18 国立大学法人三重大学 外来性ｇｉｔｒリガンド発現細胞
WO2010031185A1 (en) 2008-09-19 2010-03-25 Protox Therapeutics Inc. Treating cancer stem cells using targeted cargo proteins
CN102224242B (zh) 2008-09-24 2014-09-24 中国科学院上海有机化学研究所 新基因簇
BRPI1007476A2 (pt) 2009-01-30 2016-02-16 Enanta Pharm Inc análogos de ciclosporina para prevenir ou tratar infecção por hepatite c
WO2010117633A1 (en) 2009-04-06 2010-10-14 Wyeth Llc Treatment regimen utilizing neratinib for breast cancer
WO2010121212A2 (en) 2009-04-17 2010-10-21 H. Lee Moffit Cancer Center And Research Institute, Inc. Indoline scaffold shp-2 inhibitors and method of treating cancer
US9163330B2 (en) 2009-07-13 2015-10-20 President And Fellows Of Harvard College Bifunctional stapled polypeptides and uses thereof
US8664186B2 (en) 2009-07-24 2014-03-04 Universite De Lorraine Stambomycin and derivatives, their production and their uses as drugs
ES2608670T3 (es) 2009-08-17 2017-04-12 Memorial Sloan-Kettering Cancer Center Derivados de 2-(pirimidin-5-il)-tiopirimidina como moduladores de Hsp70 y Hsc70 para el tratamiento de trastornos proliferativos
LT3023438T (lt) 2009-09-03 2020-05-11 Merck Sharp & Dohme Corp. Anti-gitr antikūnai
CA2774973A1 (en) 2009-09-22 2011-03-31 Aileron Therapeutics, Inc. Peptidomimetic macrocycles
US20120208720A1 (en) 2009-10-22 2012-08-16 Kenji Kashiwagi Rapid display method in translational synthesis of peptide
GB0919054D0 (en) 2009-10-30 2009-12-16 Isis Innovation Treatment of obesity
CN105693861A (zh) 2009-12-29 2016-06-22 新兴产品开发西雅图有限公司 异二聚体结合蛋白及其应用
EP2533784B1 (en) 2010-02-09 2015-04-22 Neurovive Pharmaceutical AB Sanglifehrin based compounds
US8637684B2 (en) 2010-05-12 2014-01-28 Wisconsin Alumni Research Foundation Tautomycetin and tautomycetin analog biosynthesis
WO2012041524A1 (en) 2010-10-01 2012-04-05 Max-Delbrück-Centrum Für Molekulare Medizin (Mdc) Hydrazonopyrazolones as protein tyrosine phosphatase inhibitors
WO2012075048A2 (en) 2010-11-30 2012-06-07 The Johns Hopkins University Hybrid cyclic libraries and screens thereof
AR084217A1 (es) 2010-12-10 2013-05-02 Gilead Sciences Inc Inhibidores macrociclicos de virus flaviviridae
US9428845B1 (en) 2010-12-28 2016-08-30 Warp Drive Bio, Inc. Identifying new therapeutic agents
MY161199A (en) 2011-03-23 2017-04-14 Amgen Inc Fused tricyclic dual inhibitors of cdk 4/6 and flt3
ES2907071T3 (es) 2011-05-19 2022-04-21 Fundacion Del Sector Publico Estatal Centro Nac De Investigaciones Oncologicas Carlos Iii F S P Cnio Compuestos macrocíclicos como inhibidores de proteína quinasas
US9260484B2 (en) 2011-06-15 2016-02-16 Ohio State Innovation Foundation Small molecule composite surfaces as inhibitors of protein-protein interactions
WO2013001310A1 (en) 2011-06-30 2013-01-03 Centro Nacional De Investigaciones Oncológicas (Cnio) Macrocyclic compounds and their use as cdk8 inhibitors
TW201311689A (zh) 2011-08-05 2013-03-16 必治妥美雅史谷比公司 作為因子ｘｉａ抑制劑之新穎巨環化合物
DE102011111991A1 (de) 2011-08-30 2013-02-28 Lead Discovery Center Gmbh Neue Cyclosporin-Derivate
WO2013039954A1 (en) 2011-09-14 2013-03-21 Sanofi Anti-gitr antibodies
EP2836482B1 (en) 2012-04-10 2019-12-25 The Regents of The University of California Compositions and methods for treating cancer
AR091279A1 (es) 2012-06-08 2015-01-21 Gilead Sciences Inc Inhibidores macrociclicos de virus flaviviridae
EA026235B1 (ru) 2012-06-08 2017-03-31 Джилид Сайэнс, Инк. Макроциклические ингибиторы вирусов flaviviridae
CA2875718A1 (en) * 2012-06-08 2013-12-12 Selcia Limited Macrocyclic inhibitors of flaviviridae viruses
PT2872157T (pt) 2012-07-12 2020-04-30 Hangzhou Dac Biotech Co Ltd Conjugados de moléculas de ligação celular com agentes citotóxicos
ES2701076T3 (es) 2012-11-24 2019-02-20 Hangzhou Dac Biotech Co Ltd Enlazadores hidrofílicos y sus usos para la conjugación de fármacos a las moléculas que se unen a las células
WO2014113584A1 (en) 2013-01-16 2014-07-24 Rhode Island Hospital Compositions and methods for the prevention and treatment of osteolysis and osteoporosis
US9745319B2 (en) 2013-03-15 2017-08-29 Araxes Pharma Llc Irreversible covalent inhibitors of the GTPase K-Ras G12C
CA2903772A1 (en) 2013-03-15 2014-09-25 Novartis Ag Antibody drug conjugates
MX364438B (es) 2013-03-15 2019-04-26 Araxes Pharma Llc Inhibidores covalentes de kras g12c.
EP2988741B1 (en) 2013-04-26 2019-11-27 Indiana University Research&Technology Corporation Hydroxyindole carboxylic acid based inhibitors for oncogenic src homology-2 domain containing protein tyrosine phosphatase-2 (shp2)
WO2014180271A1 (zh) 2013-05-10 2014-11-13 苏州明锐医药科技有限公司 阿法替尼及其中间体的制备方法
EP2806274A1 (en) 2013-05-24 2014-11-26 AIT Austrian Institute of Technology GmbH Lung cancer diagnostic method and means
CA2953482A1 (en) 2013-07-03 2015-01-08 Indiana University Research & Technology Corporation Shp2 inhibitors and methods of treating autoimmune and/or glomerulonephritis-associated diseases using shp2 inhibitors
EP2826586A1 (en) 2013-07-18 2015-01-21 Siemens Aktiengesellschaft A method and a system for machining an object
BR112016008016B8 (pt) 2013-10-10 2023-09-26 Araxes Pharma Llc Compostos inibidores de kras g12c, composição farmacêutica compreendendo ditos compostos, métodos para regular a atividade e para preparar uma proteína mutante kras, hras ou nras g12c, método para inibir a proliferação de uma população de células e usos terapêuticos dos ditos compostos
JP6523303B2 (ja) 2014-01-17 2019-05-29 ノバルティス アーゲー Ｓｈｐ２の活性を阻害するための１−ピリダジン／トリアジン−３−イル−ピペラジン／ピペリジン／ピロリジン誘導体およびその組成物
JP6473457B2 (ja) 2014-01-17 2019-02-20 ノバルティス アーゲー Ｓｈｐ２の活性を阻害するための１−（トリアジン−３−イル／ピリダジン−３−イル）−ピペリジン／ピペラジン誘導体およびその組成物
US10233431B2 (en) 2014-02-26 2019-03-19 The Regents Of The University Of California Producing 3-hydroxycarboxylic acid and ketone using polyketide synthases
WO2015132784A1 (en) 2014-03-03 2015-09-11 Yissum Research Development Company Of The Hebrew University Of Jerusalem Ltd. Method and device for detection of pseudomonas aeruginosa
US10011600B2 (en) 2014-09-25 2018-07-03 Araxes Pharma Llc Methods and compositions for inhibition of Ras
EP3197870B1 (en) 2014-09-25 2020-08-19 Araxes Pharma LLC Inhibitors of kras g12c mutant proteins
TW201629069A (zh) 2015-01-09 2016-08-16 霍普驅動生物科技股份有限公司 參與協同結合之化合物及其用途
US10533016B2 (en) 2015-01-09 2020-01-14 Revolution Medicines, Inc. Compounds that participate in cooperative binding and uses thereof
EP3277704A1 (en) 2015-03-31 2018-02-07 Allergan, Inc. Cyclosporins modified on the mebmt sidechain by heterocyclic rings
EA201792214A1 (ru) 2015-04-10 2018-01-31 Араксис Фарма Ллк Соединения замещенного хиназолина
ES2856880T3 (es) 2015-04-15 2021-09-28 Araxes Pharma Llc Inhibidores tricíclicos condensados de KRAS y métodos de uso de los mismos
WO2016191328A1 (en) 2015-05-22 2016-12-01 Allosta Pharmaceuticals Methods to prepare and employ binding site models for modulation of phosphatase activity and selectivity determination
WO2016196591A1 (en) 2015-06-01 2016-12-08 Indiana University Research & Technology Corporation Protein tyrosine phosphatases or shp2 inhibitors and uses thereof
CN112625028A (zh) 2015-06-19 2021-04-09 诺华股份有限公司 用于抑制shp2活性的化合物和组合物
EP3310779B1 (en) 2015-06-19 2019-05-08 Novartis AG Compounds and compositions for inhibiting the activity of shp2
JP6878316B2 (ja) 2015-06-19 2021-05-26 ノバルティス アーゲー Ｓｈｐ２の活性を阻害するための化合物および組成物
EP3325447A1 (en) 2015-07-22 2018-05-30 Araxes Pharma LLC Substituted quinazoline compounds and their use as inhibitors of g12c mutant kras, hras and/or nras proteins
WO2017058728A1 (en) 2015-09-28 2017-04-06 Araxes Pharma Llc Inhibitors of kras g12c mutant proteins
EP3356347A1 (en) 2015-09-28 2018-08-08 Araxes Pharma LLC Inhibitors of kras g12c mutant proteins
EP3356354A1 (en) 2015-09-28 2018-08-08 Araxes Pharma LLC Inhibitors of kras g12c mutant proteins
EP3356351A1 (en) 2015-09-28 2018-08-08 Araxes Pharma LLC Inhibitors of kras g12c mutant proteins
EP3356349A1 (en) 2015-09-28 2018-08-08 Araxes Pharma LLC Inhibitors of kras g12c mutant proteins
US10882847B2 (en) 2015-09-28 2021-01-05 Araxes Pharma Llc Inhibitors of KRAS G12C mutant proteins
WO2017058902A1 (en) 2015-09-28 2017-04-06 Araxes Pharma Llc Inhibitors of kras g12c mutant proteins
EP4242304A3 (en) 2015-10-01 2024-02-07 Revolution Medicines, Inc. Methods and reagents for analyzing protein-protein interfaces
WO2017078499A2 (ko) 2015-11-06 2017-05-11 경북대학교 산학협력단 단백질 타이로신 탈인산화효소 억제제를 포함하는 신경염증성 질환의 예방 또는 치료용 조성물
US11008372B2 (en) 2015-11-07 2021-05-18 Board Of Regents, The University Of Texas System Targeting proteins for degradation
AU2016355433C1 (en) 2015-11-16 2021-12-16 Araxes Pharma Llc 2-substituted quinazoline compounds comprising a substituted heterocyclic group and methods of use thereof
WO2017100279A1 (en) 2015-12-09 2017-06-15 West Virginia University Chemical compound for inhibition of shp2 function and for use as an anti-cancer agent
WO2017100546A1 (en) 2015-12-09 2017-06-15 Araxes Pharma Llc Methods for preparation of quinazoline derivatives
WO2017156397A1 (en) 2016-03-11 2017-09-14 Board Of Regents, The University Of Texas Sysytem Heterocyclic inhibitors of ptpn11
WO2017172979A1 (en) 2016-03-30 2017-10-05 Araxes Pharma Llc Substituted quinazoline compounds and methods of use
ES2863873T3 (es) 2016-05-18 2021-10-11 Mirati Therapeutics Inc Inhibidores de KRAS G12C
CN109475531B (zh) 2016-05-31 2021-08-17 得克萨斯州立大学董事会 Ptpn11的杂环抑制剂
KR20220124275A (ko) 2016-06-07 2022-09-13 자코바이오 파마슈티칼스 컴퍼니 리미티드 Shp2 억제제로서 유용한 신규한 헤테로환형 유도체
CR20190063A (es) 2016-07-12 2019-05-27 Revolution Medicines Inc 3-metil pirazinas 2,5-disustituídas y 3-metil pirazinas 2,5,6-trisustituídas como inhibidores alostéricos de shp2
EP3519402A1 (en) 2016-09-29 2019-08-07 Araxes Pharma LLC Inhibitors of kras g12c mutant proteins
JP2019534260A (ja) 2016-10-07 2019-11-28 アラクセス ファーマ エルエルシー Ｒａｓの阻害剤としての複素環式化合物およびその使用方法
CA3042231A1 (en) 2016-10-28 2018-05-03 Ginkgo Bioworks, Inc. Compositions and methods for the production of compounds
KR20190077476A (ko) 2016-11-18 2019-07-03 뉴로바이브 파마슈티컬 에이비 상글리페린 거대고리 유사체의 항암 화합물로서의 용도
RU2019121922A (ru) 2016-12-15 2021-01-18 Дзе Риджентс Оф Дзе Юниверсити Оф Калифорния Композиции и способы лечения рака
KR20230150408A (ko) 2016-12-22 2023-10-30 암젠 인크 폐암, 췌장암 또는 대장암을 치료하기 위한 kras g12c 억제제로서의 벤즈이소티아졸, 이소티아졸로[3,4-b]피리딘, 퀴나졸린, 프탈라진, 피리도[2,3-d]피리다진 및 피리도[2,3-d]피리미딘 유도체
WO2018129402A1 (en) 2017-01-06 2018-07-12 Oregon Health & Science University Compositions and methods used in diagnosing and treating colorectal cancer
ES2964956T3 (es) 2017-01-10 2024-04-10 Novartis Ag Combinación farmacéutica que comprende un inhibidor de ALK y un inhibidor de SHP2
MX2019008696A (es) 2017-01-23 2019-09-13 Revolution Medicines Inc Compuestos de piridina como inhibidores de shp2 alostericos.
AR110740A1 (es) 2017-01-23 2019-05-02 Revolution Medicines Inc Compuestos bicíclicos como inhibidores alostéricos de shp2
EP3573964A1 (en) 2017-01-26 2019-12-04 Araxes Pharma LLC Benzothiophene and benzothiazole compounds and methods of use thereof
EP3573954A1 (en) 2017-01-26 2019-12-04 Araxes Pharma LLC Fused bicyclic benzoheteroaromatic compounds and methods of use thereof
WO2018140514A1 (en) 2017-01-26 2018-08-02 Araxes Pharma Llc 1-(6-(3-hydroxynaphthalen-1-yl)quinazolin-2-yl)azetidin-1-yl)prop-2-en-1-one derivatives and similar compounds as kras g12c inhibitors for the treatment of cancer
CN110382482A (zh) 2017-01-26 2019-10-25 亚瑞克西斯制药公司 稠合的杂-杂二环化合物及其使用方法
US11279689B2 (en) 2017-01-26 2022-03-22 Araxes Pharma Llc 1-(3-(6-(3-hydroxynaphthalen-1-yl)benzofuran-2-yl)azetidin-1 yl)prop-2-en-1-one derivatives and similar compounds as KRAS G12C modulators for treating cancer
JP2020505395A (ja) 2017-01-26 2020-02-20 アラクセス ファーマ エルエルシー 縮合ｎ−複素環式化合物およびその使用方法
JOP20190186A1 (ar) 2017-02-02 2019-08-01 Astellas Pharma Inc مركب كينازولين
EP3589647A1 (en) 2017-02-28 2020-01-08 Novartis AG Shp inhibitor compositions and uses for chimeric antigen receptor therapy
MX2019011330A (es) 2017-03-23 2020-02-05 Jacobio Pharmaceuticals Co Ltd Derivados heterocíclicos novedosos útiles como inhibidores de sph2.
KR20200003803A (ko) 2017-04-05 2020-01-10 레볼루션 메디슨즈, 인크. 협동 결합에 참여하는 화합물 및 그의 용도
KR20200003802A (ko) 2017-04-05 2020-01-10 레볼루션 메디슨즈, 인크. 단백질-단백질 계면을 분석하기 위한 방법 및 시약
US10800787B2 (en) 2017-04-20 2020-10-13 Apotex Inc. Process for the preparation of acalabrutinib
AU2018263886C1 (en) 2017-05-02 2022-12-22 Revolution Medicines, Inc. Rapamycin analogs as mTOR inhibitors
CA3061650A1 (en) 2017-05-11 2018-11-15 Astrazeneca Ab Heteroaryl compounds that inhibit g12c mutant ras proteins
JOP20190272A1 (ar) 2017-05-22 2019-11-21 Amgen Inc مثبطات kras g12c وطرق لاستخدامها
US11639346B2 (en) 2017-05-25 2023-05-02 Araxes Pharma Llc Quinazoline derivatives as modulators of mutant KRAS, HRAS or NRAS
TW201906832A (zh) 2017-05-25 2019-02-16 美商亞瑞克西斯製藥公司 用於癌症治療之化合物及其使用方法
BR112019024674A2 (pt) 2017-05-25 2020-06-16 Araxes Pharma Llc Inibidores covalentes da kras
EP3678703A1 (en) 2017-09-07 2020-07-15 Revolution Medicines, Inc. Shp2 inhibitor compositions and methods for treating cancer
TWI731264B (zh) 2017-09-08 2021-06-21 美商安進公司 Kras g12c抑制劑以及其使用方法
CN111201223A (zh) 2017-09-11 2020-05-26 克鲁松制药公司 SHP2的八氢环戊二烯并[c]吡咯别构抑制剂
US10689377B2 (en) 2017-11-15 2020-06-23 Mirati Therapeutics, Inc. KRas G12C inhibitors
TW201938561A (zh) 2017-12-08 2019-10-01 瑞典商阿斯特捷利康公司 化學化合物
TW201942115A (zh) 2018-02-01 2019-11-01 美商輝瑞股份有限公司 作為抗癌藥之經取代的喹唑啉和吡啶並嘧啶衍生物
TW201942116A (zh) 2018-02-09 2019-11-01 美商輝瑞股份有限公司 作為抗癌劑之四氫喹唑啉衍生物
CR20200578A (es) 2018-05-01 2021-02-22 Revolution Medicines Inc Análogos de rapamicina a c40, c28 y c32 como inhibidores de mtor
JP7381492B2 (ja) 2018-05-01 2023-11-15 レヴォリューション・メディスンズ，インコーポレイテッド Ｍｔｏｒ阻害剤としてのｃ２６－連結ラパマイシン類似体
CA3099118A1 (en) 2018-05-04 2019-11-07 Amgen Inc. Kras g12c inhibitors and methods of using the same
JP7266043B2 (ja) 2018-05-04 2023-04-27 アムジエン・インコーポレーテツド ＫＲａｓ Ｇ１２Ｃ阻害剤及びそれを使用する方法
WO2019217307A1 (en) 2018-05-07 2019-11-14 Mirati Therapeutics, Inc. Kras g12c inhibitors
TW202012415A (zh) 2018-05-08 2020-04-01 瑞典商阿斯特捷利康公司 化學化合物
MA52564A (fr) 2018-05-10 2021-03-17 Amgen Inc Inhibiteurs de kras g12c pour le traitement du cancer
JP7360396B2 (ja) 2018-06-01 2023-10-12 アムジエン・インコーポレーテツド Ｋｒａｓ ｇ１２ｃ阻害剤及び同一物の使用方法
MX2020012204A (es) 2018-06-11 2021-03-31 Amgen Inc Inhibidores de kras g12c para tratar el cáncer.
US11285156B2 (en) 2018-06-12 2022-03-29 Amgen Inc. Substituted piperazines as KRAS G12C inhibitors
CN112584833A (zh) 2018-08-01 2021-03-30 亚瑞克西斯制药公司 杂环螺化合物及其用于治疗癌症的使用方法
KR102495687B1 (ko) 2018-08-16 2023-02-07 에프. 호프만-라 로슈 아게 융합 고리 화합물
WO2020047192A1 (en) 2018-08-31 2020-03-05 Mirati Therapeutics, Inc. Kras g12c inhibitors
MA55136A (fr) 2018-11-19 2022-02-23 Amgen Inc Inhibiteurs de kras g12c et leurs procédés d'utilisation
SG11202106605VA (en) 2018-12-21 2021-07-29 Revolution Medicines Inc Compounds that participate in cooperative binding and uses thereof
CA3159559A1 (en) 2019-11-04 2021-05-14 Revolution Medicines, Inc. Ras inhibitors
JP2022553858A (ja) 2019-11-04 2022-12-26 レボリューション メディシンズ インコーポレイテッド Ｒａｓ阻害剤
US11608346B2 (en) 2019-11-04 2023-03-21 Revolution Medicines, Inc. Ras inhibitors
JP2023505100A (ja) 2019-11-27 2023-02-08 レボリューション メディシンズ インコーポレイテッド 共有ｒａｓ阻害剤及びその使用
MX2023002248A (es) 2020-09-03 2023-05-16 Revolution Medicines Inc Uso de inhibidores de sos1 para tratar neoplasias malignas con mutaciones de shp2.
CR20230165A (es) 2020-09-15 2023-06-02 Revolution Medicines Inc Derivados indólicos como inhibidores de ras en el tratamiento del cáncer
BR112023022819A2 (pt) 2021-05-05 2024-01-16 Revolution Medicines Inc Compostos, composição farmacêutica, conjugados e métodos para tratar câncer em um sujeito, para tratar um distúrbio e para inibir uma proteína ras em uma célula

Also Published As

Publication number Publication date
CA3159561A1 (en) 2021-05-14
TW202132316A (zh) 2021-09-01
CL2023000974A1 (es) 2023-09-29
US20210130303A1 (en) 2021-05-06
US11952352B2 (en) 2024-04-09
JP2022553858A (ja) 2022-12-26
CO2022006033A2 (es) 2022-07-29
KR20220109408A (ko) 2022-08-04
CN114786777A (zh) 2022-07-22
WO2021091982A1 (en) 2021-05-14
EP4054719A1 (en) 2022-09-14
BR112022008565A2 (pt) 2022-08-09
US11566007B2 (en) 2023-01-31
AU2020379734A1 (en) 2022-05-05
IL292644A (en) 2022-07-01
CN115894606A (zh) 2023-04-04
PE20221278A1 (es) 2022-09-05
US20230234929A1 (en) 2023-07-27
MX2022005359A (es) 2022-06-02

Similar Documents

Publication Publication Date Title
CR20220240A (es) Inhibidores de ras
CR20220243A (es) Inhibidores de ras
MX2022005359A (es) Inhibidores de ras.
CR20230165A (es) Derivados indólicos como inhibidores de ras en el tratamiento del cáncer
MX2021007468A (es) Compuestos que participan en la union cooperativa y usos de los mismos.
CR20230570A (es) Inhibidores de ras
CR20230558A (es) Inhibidores de ras para el tratamiento del cáncer
MX2022015272A (es) Inhibidores de la proteina kras g12c y usos de estos.
EP4295846A3 (en) Heteroarylaminopyrimidine amide autophagy inhibitors and methods of use thereof
BR112018008326A2 (pt) composições e métodos para o tratamento de câncer
JOP20220083A1 (ar) حلقات غير متجانسة ثنائية الحلقة كمثبطات لـ fgfr
AU2018278311A1 (en) IRE1 small molecule inhibitors
MX2021001807A (es) Combinacion de un inhibidor de histona desacetilasa y un inhibidor de proteina cinasa y uso farmaceutico de la misma.
MX2019010040A (es) Composiciones y métodos para el tratamiento del cáncer.
MX2023002507A (es) Inhibidores de cd73.
TR201902686T4 (tr) Aurora A kinaz inhibitörü.
MX2018006190A (es) Antibioticos de amplio espectro macrociclico.
MX2018006199A (es) Antibioticos de amplio espectro macrociclico.
MX2018013573A (es) Ciertos inhibidores de la proteína cinasa.
WO2019067498A3 (en) Peptide antibiotic complexes and methods of use thereof
MX2020011027A (es) Constructos de anticuerpos biespecíficos trivalentes.
MX2021015333A (es) Combinaciones de inhibidores para el tratamiento de enfermedades relacionadas con la expresion de dux4.
WO2020102243A3 (en) In-flow photooxygenation of aminothienopyridinones generates novel ptp4a3 phosphatase inhibitors
LV15503A (lv) 2H-selenofēn[3,2-h]hromēni izmantošanai vēža profilaksē un ārstēšanā
MX2021013117A (es) Composiciones y metodos para el tratamiento del cancer.